Formulation: A solid
Formal Name: cyclic (4→13)-disulfide L-arginyl-L-arginyl-3-(2-naphthalenyl)-L-alanyl-L-cysteinyl-L-tyrosyl-N5-(aminocarbonyl)-L-ornithyl-L-lysyl-N5-(aminocarbonyl)-D-ornithyl-L-prolyl-L-tyrosyl-L-arginyl-N5-(aminocarbonyl)-L-ornithyl-L-cysteinyl-L-argininamide, hydrochloride
Purity: ≥95%
Formula Markup: C90H140N34O19S2 • XHCl
Formula Weight: 2066,4
Shelf life (days): 1460
Notes: TC 14012 is a peptidomimetic antagonist of chemokine (C-X-C motif) receptor 4 (CXCR4; IC50 = 2.9 nM) and CXCR7 agonist.{21627,54472} It induces β-arrestin recruitment in HEK293T cells expressing CXCR7 (EC50 = 350 nM).{21627} TC 14012 reduces the cytopathic effect of HIV in infected MT-4 cells (EC50 = 0.4 nM) and inhibits HIV entry in vitro in a CXCR4-dependent manner (IC50 = 19.3 nM).{21628} It inhibits migration induced by chemokine (C-X-C motif) ligand 12 (CXCL12) in MDA-MB-231 breast cancer cells and human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 10 to 1,000 nM.{54472} TC 14012 (10 mg/kg) decreases infarct size in a mouse model of acute myocardial infarction induced by left anterior descending (LAD) coronary artery ligation.{69391}
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